EP3517535A4 - ALKYNYL-SUBSTITUTED HETEROCYCLIC COMPOUND, PRODUCTION METHOD THEREFOR, AND MEDICAL USE THEREOF - Google Patents

ALKYNYL-SUBSTITUTED HETEROCYCLIC COMPOUND, PRODUCTION METHOD THEREFOR, AND MEDICAL USE THEREOF Download PDF

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Publication number
EP3517535A4
EP3517535A4 EP17849992.7A EP17849992A EP3517535A4 EP 3517535 A4 EP3517535 A4 EP 3517535A4 EP 17849992 A EP17849992 A EP 17849992A EP 3517535 A4 EP3517535 A4 EP 3517535A4
Authority
EP
European Patent Office
Prior art keywords
alkynyl
production method
heterocyclic compound
substituted heterocyclic
method therefor
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP17849992.7A
Other languages
German (de)
French (fr)
Other versions
EP3517535A1 (en
EP3517535B1 (en
Inventor
Xiangyang Chen
Yingxiang GAO
Norman Xianglong Kong
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Beijing Innocare Pharma Tech Co Ltd
Original Assignee
Beijing Innocare Pharma Tech Co Ltd
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Filing date
Publication date
Application filed by Beijing Innocare Pharma Tech Co Ltd filed Critical Beijing Innocare Pharma Tech Co Ltd
Publication of EP3517535A1 publication Critical patent/EP3517535A1/en
Publication of EP3517535A4 publication Critical patent/EP3517535A4/en
Application granted granted Critical
Publication of EP3517535B1 publication Critical patent/EP3517535B1/en
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/44—Oxygen and nitrogen or sulfur and nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
EP17849992.7A 2016-09-19 2017-01-25 Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use thereof Active EP3517535B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201610833890.3A CN107840842A (en) 2016-09-19 2016-09-19 Alkynes is for heterocyclic compound, its preparation method and its in application pharmaceutically
PCT/CN2017/072570 WO2018049781A1 (en) 2016-09-19 2017-01-25 Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use thereof

Publications (3)

Publication Number Publication Date
EP3517535A1 EP3517535A1 (en) 2019-07-31
EP3517535A4 true EP3517535A4 (en) 2020-02-26
EP3517535B1 EP3517535B1 (en) 2022-06-29

Family

ID=61618562

Family Applications (1)

Application Number Title Priority Date Filing Date
EP17849992.7A Active EP3517535B1 (en) 2016-09-19 2017-01-25 Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use thereof

Country Status (12)

Country Link
US (3) US10710981B2 (en)
EP (1) EP3517535B1 (en)
JP (1) JP6906811B2 (en)
KR (1) KR102783517B1 (en)
CN (2) CN107840842A (en)
AU (1) AU2017327954B2 (en)
CA (1) CA3036594C (en)
ES (1) ES2925212T3 (en)
MX (1) MX390747B (en)
RU (1) RU2729069C1 (en)
SG (1) SG10202102822RA (en)
WO (1) WO2018049781A1 (en)

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WO2020120673A1 (en) * 2018-12-13 2020-06-18 Intervet International B.V. Process for preparing 1-[(3r,4s)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl)amino]p yrazole-4-carboxamide
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
KR20220098759A (en) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) A method of treating cancer that has acquired resistance to a kinase inhibitor
AU2020412067A1 (en) * 2019-12-26 2022-08-11 Beijing Innocare Pharma Tech Co., Ltd. Crystalline forms of (S) -1- (1-acryloylpyrrolidin-3-yl) -3- ( (3, 5-dimethoxyphenyl) ethynyl) -5- (methylamino) -1H-pyrazole-4-carboxamide
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN116057045A (en) * 2020-06-05 2023-05-02 金耐特生物制药公司 Fibroblast Growth Factor Receptor Kinase Inhibitors
CN116096707A (en) * 2020-06-05 2023-05-09 金耐特生物制药公司 Inhibitors of fibroblast growth factor receptor kinase
WO2022042613A1 (en) * 2020-08-27 2022-03-03 上海和誉生物医药科技有限公司 1h-pyrazol-4-amide derivative, preparation method therefor, and use thereof
CA3204407A1 (en) * 2021-01-12 2022-07-21 Yucheng PANG Process for preparing (s)-1-(1-acryloylpyrrolidin-3-yl)-3-((3,5-dimethoxyphenyl) ethynyl)-5-(methylamino)-1h-pyrazole-4-carboxamide
CN115433190B (en) * 2021-06-02 2024-09-20 药雅科技(上海)有限公司 Preparation method and application of irreversible heterocyclic compound FGFR inhibitor
CN114853739B (en) * 2021-02-03 2023-09-22 药雅科技(上海)有限公司 Acetylenic pyrazine FGFR inhibitor and preparation method and application thereof
CN115043832B (en) * 2021-03-08 2023-08-22 药雅科技(上海)有限公司 FGFR inhibitor acetylenic heterocyclic compound and preparation method and application thereof
JP2024539723A (en) * 2021-11-03 2024-10-29 ベイジン・イノケア・ファーマ・テク・カンパニー・リミテッド Amorphous solid dispersion comprising (S)-1-(1-acryloylpyrrolidin-3-yl)-3-((3,5-dimethoxyphenyl)ethynyl)-5-(methylamino)-1H-pyrazole-4-carboxamide
CA3238193A1 (en) * 2021-11-16 2023-05-25 Jisong Cui Method for treating head and neck cancer
KR20240119095A (en) * 2021-12-08 2024-08-06 킨네이트 바이오파마 인크. Solid State Forms of FGFR Inhibitors
WO2023107870A1 (en) * 2021-12-08 2023-06-15 Kinnate Biopharma Inc. Inhibitors of fibroblast growth factor receptor kinases
EP4444713A4 (en) * 2021-12-08 2025-08-06 Kinnate Biopharma Inc Treating cancer with an FGFR kinase inhibitor

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Also Published As

Publication number Publication date
CN109843873B (en) 2022-06-17
MX2019003143A (en) 2019-06-17
WO2018049781A1 (en) 2018-03-22
EP3517535A1 (en) 2019-07-31
JP2019529444A (en) 2019-10-17
ES2925212T3 (en) 2022-10-14
US20190210997A1 (en) 2019-07-11
EP3517535B1 (en) 2022-06-29
CN109843873A (en) 2019-06-04
US20200339541A1 (en) 2020-10-29
JP6906811B2 (en) 2021-07-21
CA3036594C (en) 2024-02-13
AU2017327954B2 (en) 2022-02-03
AU2017327954A1 (en) 2019-05-02
US11059805B2 (en) 2021-07-13
US10710981B2 (en) 2020-07-14
RU2729069C1 (en) 2020-08-04
MX390747B (en) 2025-03-21
KR20190052113A (en) 2019-05-15
US11572353B2 (en) 2023-02-07
US20210332027A1 (en) 2021-10-28
CN107840842A (en) 2018-03-27
SG10202102822RA (en) 2021-05-28
CA3036594A1 (en) 2018-03-22
KR102783517B1 (en) 2025-03-19

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